FR900359 and Asthma

Heterotrimeric G proteins are molecular switches in GPCR signaling pathways and regulate a plethora of physiological and pathological processes. GPCRs are efficient drug targets, and more than 30% of the drugs in use target them. However, selectively targeting an individual GPCR may be undesirable in various multifactorial diseases in which multiple receptors are involved. In addition, abnormal activation or expression of G proteins is frequently associated with diseases. Furthermore, G proteins harboring mutations often result in malignant diseases. Thus, targeting G proteins instead of GPCRs might provide alternative approaches for combating these diseases. In this review, we discuss the biochemistry of heterotrimeric G proteins, describe the G protein-associated diseases, and summarize the currently known modulators that can regulate the activities of G proteins. The outlook for targeting G proteins to treat diverse diseases is also included in this manuscript.

Topics: Animals; Asthma; Bacterial Toxins; Drug Delivery Systems; Drug Discovery; Heart Failure; Heterotrimeric GTP-Binding Proteins; Humans; Neoplasms; Peptides, Cyclic; Protein Structure, Secondary; Receptors, G-Protein-Coupled; Signal Transduction; Thrombosis

Obstructive lung diseases are common causes of disability and death worldwide. A hallmark feature is aberrant activation of G

Topics: Animals; Asthma; Bronchoconstriction; Depsipeptides; Disease Models, Animal; GTP-Binding Protein alpha Subunits, Gq-G11; Humans; Lung; Mice; Muscle Relaxation; Myocytes, Smooth Muscle; Ovalbumin; Pneumonia; Pyroglyphidae; Signal Transduction; Sus scrofa